Assay Detail
Binding
CHEMBL3593134
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Inhibition of MEK U911-activated ERK2 (unknown origin) using Erktide as substrate preincubated with enzyme for 20 mins prior to substrate addition by RapidFire Mass Spectrometry in presence of ATP at Km concentration
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 7.11 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3590120 | — | — | 1 | 8.51 |
| CHEMBL3590121 | — | — | 1 | 8.16 |
| CHEMBL3590110 | — | — | 1 | 8.12 |
| CHEMBL3590118 | — | — | 1 | 8.07 |
| CHEMBL3590123 | — | — | 1 | 8.00 |
| CHEMBL3590125 | — | — | 1 | 7.41 |
| CHEMBL3590116 | — | — | 1 | 7.40 |
| CHEMBL3590117 | — | — | 1 | 7.38 |
| CHEMBL3590114 | — | — | 1 | 7.36 |
| CHEMBL3590111 | — | — | 1 | 7.13 |
| CHEMBL3590122 | — | — | 1 | 7.11 |
| CHEMBL3590124 | — | — | 1 | 7.07 |
| CHEMBL3590115 | — | — | 1 | 6.58 |
| CHEMBL3590113 | — | — | 1 | 6.55 |
| CHEMBL3590109 | — | — | 1 | 6.43 |
| CHEMBL3590119 | — | — | 1 | 6.32 |
| CHEMBL3590108 | — | — | 1 | 5.29 |
| CHEMBL3590112 | — | — | 1 | 5.05 |
| CHEMBL3590107 | — | — | 1 | - |
| CHEMBL3590106 | ULIXERTINIB | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3590120 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL3590121 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL3590110 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL3590118 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL3590123 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL3590125 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3590116 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3590117 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL3590114 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL3590111 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL3590122 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL3590124 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL3590115 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL3590113 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL3590109 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL3590119 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL3590108 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL3590112 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL3590107 | — | IC50 | < | 0.3 | nM | - |
| CHEMBL3590106 | ULIXERTINIB | IC50 | < | 0.3 | nM | - |